Drug intelligence / Profile preview

balovaptan + rifampicin

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

**balovaptan + rifampicin** is a combination of two small molecule pharmaceuticals: **balovaptan**, a highly selective, competitive antagonist of the vasopressin V1A receptor, and **rifampicin**, a broad-spectrum antibiotic in the rifamycin class. Balovaptan was developed primarily for neurobehavioral indications such as autism spectrum disorder (ASD) and post-traumatic stress disorder (PTSD), acting via inhibition of the V1A receptor to modulate social behavior-related neural circuits[1][2][5][7]. It is highly selective (>6000-fold over V2 and >2600-fold over oxytocin receptor) and is mainly metabolized by CYP3A4[3]. Clinical development for ASD and PTSD reached late-stage but did not show significant efficacy for core ASD symptoms[2][3][6][7]. **Rifampicin** is a bactericidal antibiotic that inhibits bacterial DNA-dependent RNA polymerase and is used primarily for tuberculosis and other bacterial infections (though not detailed in the cited results, this information is widely established). The combination of **balovaptan + rifampicin** is not itself a marketed pharmaceutical product; any reference would likely pertain to their co-administration, which is pharmacokinetically relevant because rifampicin is a strong CYP3A4 inducer and can thereby substantially reduce plasma concentrations and exposure of drugs like balovaptan that are metabolized by CYP3A4[3].

02

Targets

AVPR1A (Arginine vasopressin receptor 1A)

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